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Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 2009, Volume 17, Issue 17, pp. 6257 - 6263
Twenty one substituted bis-indole compounds were designed, synthesized and tested on five kinases involved in Alzheimer’s disease: CDK1/cyclin B, CDK5/p25,... 
Casein kinase 1 | DYRK1A | Indirubin | Alzheimer’s disease | Glycogen synthase kinase-3 | Cyclin-dependent kinases | Alzheimer's disease | CONSTITUENT | CHEMISTRY, MEDICINAL | CANCER CELLS | INDIRUBINS | PHOSPHORYLATION | BIOCHEMISTRY & MOLECULAR BIOLOGY | RECEPTOR-LIGAND | CHEMISTRY, ORGANIC | INDUCTION | PROTEIN-KINASES | POTENT | TYRIAN PURPLE | Protein Kinases - metabolism | Protein-Tyrosine Kinases - metabolism | Humans | Indoles - chemical synthesis | Protein Kinases - chemistry | Cyclin B1 - metabolism | Protein Kinase Inhibitors - chemistry | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Casein Kinase I - antagonists & inhibitors | Protein-Serine-Threonine Kinases - metabolism | Protein Kinase Inhibitors - chemical synthesis | Neuroprotective Agents - chemistry | Glycogen Synthase Kinase 3 - antagonists & inhibitors | Alzheimer Disease - drug therapy | Indoles - toxicity | Neuroprotective Agents - toxicity | Glycogen Synthase Kinase 3 - metabolism | Cyclin-Dependent Kinase 5 - metabolism | Cyclin-Dependent Kinase 5 - antagonists & inhibitors | Neuroprotective Agents - chemical synthesis | Protein Kinase Inhibitors - toxicity | Casein Kinase I - metabolism | Cyclin B1 - antagonists & inhibitors | Indoles - chemistry | Protein-Tyrosine Kinases - antagonists & inhibitors | Synthesis | Casein | Glycogen | Phosphotransferases | Index Medicus | Life Sciences | Cellular Biology
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 04/2013, Volume 23, Issue 7, pp. 2007 - 2013
The design and synthesis of pyridazinone and phthalazinone derivatives are described. Newly synthesized compounds were tested on a panel of four kinases in... 
Phthalazinone | Docking | Pyridazinone | Kinases | GSK3 | CHEMISTRY, MEDICINAL | SAR | ALZHEIMERS-DISEASE | GLYCOGEN-SYNTHASE KINASE-3 | GSK-3-BETA | CHEMISTRY, ORGANIC | THIADIAZOLIDINONE DERIVATIVES | CYCLIN-DEPENDENT KINASES | POTENT | PHARMACOLOGICAL INHIBITORS | STRUCTURAL REQUIREMENTS | Phthalazines - chemical synthesis | Protein-Tyrosine Kinases - metabolism | Antineoplastic Agents - chemical synthesis | Humans | Structure-Activity Relationship | Phthalazines - chemistry | Pyridazines - pharmacology | Pyridazines - chemical synthesis | Dose-Response Relationship, Drug | Protein Kinase Inhibitors - chemistry | Drug Design | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Casein Kinase I - antagonists & inhibitors | Antineoplastic Agents - pharmacology | Molecular Structure | Protein-Serine-Threonine Kinases - metabolism | Protein Kinase Inhibitors - chemical synthesis | Glycogen Synthase Kinase 3 - antagonists & inhibitors | HCT116 Cells | Models, Molecular | Antineoplastic Agents - chemistry | Glycogen Synthase Kinase 3 - metabolism | Cyclin-Dependent Kinase 5 - metabolism | Pyridazines - chemistry | Phthalazines - pharmacology | Cyclin-Dependent Kinase 5 - antagonists & inhibitors | Cell Line, Tumor | HL-60 Cells | Casein Kinase I - metabolism | Cell Proliferation - drug effects | Protein Kinase Inhibitors - pharmacology | Drug Screening Assays, Antitumor | Protein-Tyrosine Kinases - antagonists & inhibitors | Drugstores | Models | Universities and colleges | Protein kinases
Journal Article
Journal Article
Molecules, ISSN 1420-3049, 07/2015, Volume 20, Issue 7, pp. 12412 - 12435
A new route to 3-(4-arylmethylamino)butyl-5-arylidene-2-thioxo-1,3-thiazolidine4-one 9 was developed in six steps from commercial 1,4-diaminobutane 1 as... 
5-arylidene rhodanine | One-pot two-steps | HsCDK5-p25 | Knoevenagel condensation | Protein kinase | Cell lines | Inhibitor | Alzheimer's disease | Cancer | SsCK1 | cell lines | PHOSPHORYLATION | ALZHEIMERS-DISEASE | CHEMISTRY, ORGANIC | protein kinase | DISCOVERY | RHODANINE DERIVATIVES | inhibitor | one-pot two-steps | PURIFICATION | BIOLOGICAL EVALUATION | cancer | AFFINITY-CHROMATOGRAPHY | INHIBITORS | LEUCETTAMINE B | IMMOBILIZED AXIN | Antineoplastic Agents, Alkylating - chemical synthesis | Thiazolidines - chemical synthesis | Casein Kinase I - genetics | Humans | Antineoplastic Agents, Alkylating - pharmacology | Glycogen Synthase Kinase 3 beta | Intracellular Signaling Peptides and Proteins - metabolism | Structure-Activity Relationship | Cyclin-Dependent Kinase 5 - genetics | Swine | Protein-Serine-Threonine Kinases - antagonists & inhibitors | Casein Kinase I - antagonists & inhibitors | Thiazolidines - pharmacology | Intracellular Signaling Peptides and Proteins - genetics | Microwaves | Protein-Serine-Threonine Kinases - metabolism | Caco-2 Cells | Protein Kinase Inhibitors - chemical synthesis | Gene Expression | Glycogen Synthase Kinase 3 - antagonists & inhibitors | HCT116 Cells | Intracellular Signaling Peptides and Proteins - antagonists & inhibitors | Thiones - chemistry | Protein-Serine-Threonine Kinases - genetics | Glycogen Synthase Kinase 3 - metabolism | Cyclin-Dependent Kinase 5 - metabolism | Cyclin-Dependent Kinase 5 - antagonists & inhibitors | Animals | Glycogen Synthase Kinase 3 - genetics | Cell Line, Tumor | Casein Kinase I - metabolism | Cell Proliferation - drug effects | Protein Kinase Inhibitors - pharmacology | Putrescine - chemistry | Aldehydes - chemistry | Life Sciences | Alzheimer’s disease
Journal Article
Cellular Physiology and Biochemistry, ISSN 1015-8987, 07/2016, Volume 39, Issue 2, pp. 584 - 595
Journal Article
Cellular Physiology and Biochemistry, ISSN 1015-8987, 2017, Volume 42, Issue 4, pp. 1575 - 1591
Background/Aims: The mammalian target of rapamycin (mTOR) inhibitor temsirolimus is utilized for the treatment of malignancy. Temsirolimus is at least in part... 
Ceramide | Eryptosis | Oxidative stress | Calcium | Staurosporine | Phosphatidylserine | PHYSIOLOGY | STIMULATION | SOLID TUMORS | SORAFENIB | RENAL-CELL CARCINOMA | ENERGY DEPLETION | PHASE-II TRIAL | IN-VIVO | INDUCED ADHESION | PHOSPHATIDYLSERINE EXPOSURE | Hemolysis - drug effects | Reactive Oxygen Species - metabolism | TOR Serine-Threonine Kinases - metabolism | Calcium - metabolism | Casein Kinase I - genetics | Humans | TOR Serine-Threonine Kinases - antagonists & inhibitors | Caspases - metabolism | TOR Serine-Threonine Kinases - genetics | Casein Kinase I - antagonists & inhibitors | Erythrocytes - cytology | Antineoplastic Agents - pharmacology | Benzamides - pharmacology | p38 Mitogen-Activated Protein Kinases - metabolism | Eryptosis - drug effects | Fluoresceins - chemistry | Sirolimus - analogs & derivatives | Ceramides - metabolism | Signal Transduction | Caspases - genetics | Xanthenes - chemistry | Phosphatidylserines - metabolism | Gene Expression Regulation | p38 Mitogen-Activated Protein Kinases - genetics | Imidazoles - pharmacology | Sirolimus - pharmacology | Benzophenanthridines - pharmacology | Eryptosis - genetics | Erythrocytes - drug effects | Annexin A5 - metabolism | p38 Mitogen-Activated Protein Kinases - antagonists & inhibitors | Erythrocytes - metabolism | Casein Kinase I - metabolism | Protein Kinase Inhibitors - pharmacology | Pyridines - pharmacology | Aniline Compounds - chemistry | Primary Cell Culture | Oligopeptides - pharmacology | Staurosporine - pharmacology
Journal Article
PLoS Pathogens, ISSN 1553-7366, 10/2012, Volume 8, Issue 10, p. e1002972
The Kaposi sarcoma associated herpesvirus (KSHV) latency associated nuclear antigen (LANA) is expressed in all KSHV associated malignancies and is essential... 
TRANSCRIPTIONAL ACTIVATION | SARCOMA-ASSOCIATED HERPESVIRUS | MICROBIOLOGY | NUCLEAR ANTIGEN INTERACTS | LYTIC REPLICATION | ENCODED LANA | VIROLOGY | MITOTIC CHROMOSOMES | PROTEIN-KINASE PATHWAYS | EPISOME PERSISTENCE | RIBOSOMAL S6 KINASE | CANCER-CELL-PROLIFERATION | PARASITOLOGY | Protein Kinases - metabolism | Chromatin - metabolism | Phosphorylation | Antigens, Viral - metabolism | Humans | Ribosomal Protein S6 Kinases, 90-kDa - metabolism | Herpesvirus 8, Human - metabolism | HEK293 Cells | Ribosomal Protein S6 Kinases, 90-kDa - antagonists & inhibitors | Casein Kinase I - antagonists & inhibitors | Protein Interaction Domains and Motifs | Binding Sites | Amino Acid Sequence | Cell Line | Glycogen Synthase Kinase 3 - antagonists & inhibitors | Antigens, Viral - chemistry | Fungal Proteins | Nuclear Proteins - metabolism | Sarcoma, Kaposi - virology | Glycogen Synthase Kinase 3 - metabolism | Nuclear Proteins - chemistry | Herpesvirus 4, Human | Mitogen-Activated Protein Kinases - antagonists & inhibitors | Casein Kinase I - metabolism | Histones - metabolism | Mitogen-Activated Protein Kinases - metabolism | Chromatin | Human herpesvirus 8 | Viral proteins | Physiological aspects | Genetic aspects | Epstein-Barr virus | Research | Virulence (Microbiology) | Health aspects | Protein binding | Proteins | Cell growth | DNA methylation | Life sciences | Genomes | Kinases | Experiments | Chromosomes
Journal Article
PLoS ONE, ISSN 1932-6203, 2011, Volume 6, Issue 5, p. e19589
Antibiotic resistance is recognized as a growing healthcare problem. To address this issue, one strategy is to thwart the causal mechanism using an adjuvant in... 
POTENT | ENZYME | PRELIMINARY CRYSTALLOGRAPHIC ANALYSIS | SUBSTRATE | MULTIDISCIPLINARY SCIENCES | ANTIBIOTIC-RESISTANCE | KINETIC MECHANISM | IIIA | PHOSPHOTRANSFERASE | SELECTIVITY | BINDING | Adjuvants, Pharmaceutic - pharmacology | Phosphotransferases (Alcohol Group Acceptor) - chemistry | Casein Kinase I - chemistry | Kanamycin Kinase - metabolism | Crystallography, X-Ray | Eukaryotic Cells - metabolism | Nucleotides - metabolism | Nucleotides - chemistry | Phosphotransferases (Alcohol Group Acceptor) - metabolism | Isoquinolines - chemistry | Kanamycin Kinase - antagonists & inhibitors | Kanamycin Kinase - chemistry | Phosphotransferases (Alcohol Group Acceptor) - antagonists & inhibitors | Protein Kinase Inhibitors - chemistry | Protein Binding - drug effects | Drug Design | Casein Kinase I - antagonists & inhibitors | Casein Kinase I - metabolism | Protein Kinase Inhibitors - pharmacology | Binding Sites | Drug resistance in microorganisms | Casein | Antibiotics | Analysis | Crystals | Glycine | Drug therapy | Structure | Health aspects | Protein kinases | Protein binding | Health care | Hydrocarbons | Casein kinase I | Homology | Aminoglycosides | Biochemistry | Kinases | Inactivation | Crystallography | Proteins | Immunology | Antibiotic resistance | Bacteria | Aminoglycoside antibiotics | Inhibition | Nosocomial infections | Adenosine triphosphate | Crystal structure | Binding | Enzymes | Deactivation | Protein kinase inhibitors | Inhibitors | Collaboration | BASIC BIOLOGICAL SCIENCES
Journal Article
Molecular & Biochemical Parasitology, ISSN 0166-6851, 2006, Volume 149, Issue 1, pp. 86 - 98
Trisubstituted pyrrole inhibitors of the essential coccidian parasite cGMP dependent protein kinase (PKG) block parasite invasion and show efficacy against in... 
cGMP-dependent protein kinase | Toxoplasma | CK1 | CDPK | Eimeria | LIGHT-CHAIN KINASE | MOLECULAR CHARACTERIZATION | HOST-CELL INVASION | APICOMPLEXAN PARASITES | BIOCHEMISTRY & MOLECULAR BIOLOGY | PROTOZOAN PARASITE | EIMERIA-TENELLA | PLASMODIUM-FALCIPARUM | CLINICAL-TRIALS | TOXOPLASMA-GONDII | GLIDING MOTILITY | PARASITOLOGY | Protein Kinases - metabolism | Skin - cytology | Coccidiostats - metabolism | Humans | Molecular Sequence Data | Eimeriida - drug effects | Male | Coccidiostats - isolation & purification | Recombinant Proteins | Toxoplasma - enzymology | Pyrimidines - metabolism | Cyclic GMP-Dependent Protein Kinases - antagonists & inhibitors | Fibroblasts | Casein Kinase I - antagonists & inhibitors | Calcium-Calmodulin-Dependent Protein Kinase Type 1 | Eimeria tenella - drug effects | Imidazoles - metabolism | Amino Acid Sequence | Pyrroles - metabolism | Eimeria tenella - enzymology | Imidazoles - pharmacology | Kidney - cytology | Epitopes | Protein Kinase Inhibitors - isolation & purification | Pyrimidines - pharmacology | Calcium-Calmodulin-Dependent Protein Kinases - antagonists & inhibitors | Pyrroles - pharmacology | Animals | Pyridines - metabolism | Casein Kinase I - metabolism | Coccidiostats - pharmacology | Protein Kinase Inhibitors - pharmacology | Pyridines - pharmacology | Toxoplasma - drug effects | Eimeriida - enzymology | Protein Kinase Inhibitors - metabolism | Enzymes | Casein | Heterocyclic compounds | Analysis | Physiological aspects | Amino acids | Thiophene | Protein kinases | Cobalt | Protein binding
Journal Article
Nature Structural and Molecular Biology, ISSN 1545-9993, 03/2018, Volume 25, Issue 3, pp. 261 - 269
Journal Article
Journal Article
Biochemical Journal, ISSN 0264-6021, 12/2007, Volume 408, Issue 3, pp. 297 - 315
The specificities of 65 compounds reported to be relatively specific inhibitors of protein kinases have been profiled against a panel of 70-80 protein kinases.... 
Drug discovery | Kinase profiling | Protein kinase | Anti-cancer drugs | Inhibitor specificity | RHO-ASSOCIATED KINASE | TUMOR PROGRESSION | FAMILY-MEMBERS | BIOCHEMISTRY & MOLECULAR BIOLOGY | CELL-PROLIFERATION | protein kinase | P38 MAP KINASE | CYCLIN-DEPENDENT KINASES | RECEPTOR TYROSINE KINASES | drug discovery | kinase profiling | SB 203580 | anti-cancer drugs | ISOFORMS IN-VITRO | P90 RSK | inhibitor specificity | Amino Acid Sequence | Cell Line | Phosphorylation | Recombinant Proteins - antagonists & inhibitors | Animals | Mitogen-Activated Protein Kinases - antagonists & inhibitors | Humans | Drug Design | Protein Kinase Inhibitors - pharmacology | Enzyme Activation | Mitogen-Activated Protein Kinases - metabolism | Spodoptera | Yes1, Yamaguchi sarcoma viral oncogene homologue 1 | CSK, C-terminal Src kinase | Lck, lymphocyte cell-specific protein-tyrosine kinase | EGF, epidermal growth factor | FGF-R, fibroblast-growth-factor receptor | PAK, p21-activated protein kinase | PDK, 3-phosphoinositide-dependent protein kinase | PI3K, phosphatidylinositol (phosphoinositide) 3-kinase | NEK, NIMA (never in mitosis in Aspergillus nidulans)-related kinase | RSK, p90 ribosomal S6 kinase | HEK-293 cells, human embryonic kidney-293 cells | VEGF, vascular endothelial growth factor (vasoendothelial growth factor) | EF2K, elongation-factor-2 kinase | CK, casein kinase | PTEN, phosphatase and tensin homologue deleted on chromosome 10 | ERK, extracellular-signal-regulated kinase | ATM, ataxia telangiectasia mutated | SRPK, serine-arginine protein kinase | IL-1, interleukin 1 | MNK, MAPK-integrating protein kinase | ROCK, Rho-dependent protein kinase | CaMKK, CaMK kinase | GST, glutathione transferase | MKK1, MAPK kinase-1 (also called MEK1, MAPK or ERK kinase 1) | GAK, cyclin G-associated kinase | FMK, fluoromethylketone | MST, mammalian homologue Ste20-like kinase | PKA, cAMP-dependent protein kinase | FKBP, FK506-binding protein | PPAR, peroxisome-proliferator-activated receptor | IKK, inhibitory κB kinase | PH, pleckstrin homology | MBP, myelin basic protein | AICAR, aminoimidazole-4-carboxamide-1-β-D-ribofuranoside | MAPKAP-K, MAPK-activated protein kinase | Sf21, Spodoptera frugiperda (fall armyworm) 21 | MARK, microtubule-affinity-regulating kinase | PIM, provirus integration site for Moloney murine leukaemia virus | LPS, lipopolysaccharide | MSK, mitogen- and stress-activated protein kinase | MAPK, mitogen-activated protein kinase | MELK, maternal embryonic leucine-zipper kinase | His6, hexahistidine | CAK, cyclin-dependent kinase-activating kinase | Eph-A2, Ephrin A2 receptor | PLK, polo-like kinase | ATF2, activating transcription factor 2 | PKD, protein kinase D | Src, sarcoma kinase | AMPK, AMP-activated protein kinase | MMS, methyl methanesulfonate | CHK, checkpoint kinase | JNK, c-Jun N-terminal kinase | TORC1, mTOR (mammalian target of rapamycin)–raptor (regulatory associated protein of mTOR) complex | BRSK, brain-specific kinase | RIP2, receptor-interacting protein 2 | IGF-1, insulin-like growth factor-1 | S6K1, S6 kinase 1 | DYRK, dual-specificity tyrosine-phosphorylated and -regulated kinase | HIPK, homeodomain-interacting protein kinase | ZMP, aminoimidazole-4-carboxamide-1-β-D-ribofuranoside monophosphate | PRAK, p38-regulated activated kinase | PKC, protein kinase C | Src-I1, Src inhibitor 1 | TANK, TRAF (tumour-necrosis-factor-receptor-associated factor)-family-member-associated nuclear factor κB activator | NFAT, nuclear factor for activated T-cells | PHK, phosphorylase kinase | GSK3, glycogen synthase kinase 3 | PKB, protein kinase B (also called Akt) | CaMK, calmodulin-dependent kinase | CDK, cyclin-dependent protein kinase | NDRG, N-myc downstream-regulated gene | SmMLCK, smooth-muscle myosin light-chain kinase | TBK1, TANK-binding kinase 1 | PRK, protein kinase C-related kinase | SGK, serum- and glucocorticoid-induced kinase
Journal Article